- New Bifunctional Chelator p-SCN-PhPr-NE3TA for Copper-64: Synthesis, Peptidomimetic Conjugation, Radiolabeling, and Evaluation for PET Imaging
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Bifunctional chelators play an important role in developing metallic radionuclide-based radiopharmaceuticals. In this study, a new bifunctional ligand, p-SCN-PhPr-NE3TA, was synthesized and conjugated to a very late antigen-4 targeting peptidomimetic, LLP2A, for evaluating its application in 64Cu-based positron emission tomography (PET) imaging. The new ligand exhibited strong selective coordination of Cu(II), leading to a robust Cu complex, even in the presence of 10-fold Fe(III). The LLP2A conjugate of p-SCN-PhPr-NE3TA was prepared and successfully labeled with 64Cu under mild conditions. The conjugate 64Cu-NE3TA-PEG4-LLP2A showed significantly higher specific activity, compared with 64Cu-NOTA-PEG4-LLP2A, while maintaining comparable serum stability. Subsequent biodistribution studies and PET imaging in mice bearing B16F10 xenografts confirmed its favorable in vivo performance and high tumor uptake with low background, rendering p-SCN-PhPr-NE3TA a promising bifunctional chelator for 64Cu-based radiopharmaceuticals.
- Gai, Yongkang,Sun, Lingyi,Hui, Wenqi,Ouyang, Qin,Anderson, Carolyn J.,Xiang, Guangya,Ma, Xiang,Zeng, Dexing
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- Synthesis and evaluation of a class of 1,4,7-triazacyclononane derivatives as iron depletion antitumor agents
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Iron depletion has been confirmed as an efficient strategy for cancer treatment. In the current study, a series of 1,4,7-triazacyclononane derivatives HE-NO2A, HP-NO2A and NE2P2A, as well as the bifunctional chelators p-NO2-PhPr-NE3TA and p-NH
- Wang, Sheng,Gai, Yongkang,Zhang, Shasha,Ke, Lei,Ma, Xiang,Xiang, Guangya
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supporting information
p. 117 - 121
(2017/12/15)
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- Synthesis method of nifekalant hydrochloride medical intermediate 2-[3-(4-nitrophenyl) propyl amino] ethyl alcohol
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The invention discloses a synthesis method of nifekalant hydrochloride medical intermediate 2-[3-(4-nitrophenyl) propyl amino] ethyl alcohol. The synthesis method comprises the following steps: adding 2-[3-(4-nitrophenyl) propionylamino] ethyl alcohol and aluminum borohydride into a trifluorothioacetate solution, adding an ethyl acetate solution drop by drop for heating reaction, then cooling, adding a butanone solution and the ethyl acetate solution to continue to carry out heating reaction, adjusting the pH value of the solution, separating out crystals, performing suction filtration, dehydrating with a dehydrating agent, washing, heating and filtration, cooling for crystallization, and performing suction filtration again and decompressed drying, so as to obtain 2-[3-(4-nitrophenyl) propyl amino] ethyl alcohol. Compared with the conventional synthesis method, the synthesis method disclosed by the invention has the advantages that the number of medium procedures of reaction is reduced, the reaction time is shortened, and the reaction yield is increased; meanwhile, a new reaction line is developed, so that the reaction yield can be further increased favorably in the later stage.
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Paragraph 0019-0023
(2017/04/04)
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- Pyrimidinedione derivatives and antiarrhythmic agents containing same
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Pyrimidinedione derivatives of the formula: STR1 wherein R1 and R2 is so linked with each other as to make an alkylene chain and thus form a heterocyclic structure, A, R3, R4, X1, X2 and X3 are substituents, respectively, and n is 2 or 3 have a basic backbone in which a phenyl group part and a pyrimidinedione part are linked by a structure comprising an alkyl chain and a heterocyclic ring having two nitrogen atoms. These compounds are useful for a medical treatment of cardiac arrhythmias.
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- Synthesis and pharmacological studies of N-substituted 6-[(2- aminoethyl)amino]-1,3-dimethyl-2,4(1H,3H)-pyrimidinediones, novel class III antiarrhythmic agents
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A series of 6-[(2-aminoethyl)amino]-1,3-dimethyl-2,4(1H,3H)- pyrimidinedione derivatives were synthesized and studied for their class III electrophysiological activity and class II (β-blocking) effects in in vitro and in vivo models. Structure-activity re
- Katakami,Yokoyama,Miyamoto,Mori,Kawauchi,Nobori,San-nohe,Kaiho,Kamiya
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p. 3325 - 3330
(2007/10/02)
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- Pyrimidinedione compounds, method of producing the same and antiarrythmic agents containing the same
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A pyrimidinedione derivative compound has a basic backbone in which a phenyl group part and a pyrimidinedione part are linked by a structure comprising an alkyl chain containing at least two nitrogen atoms. The pyrimidinedione derivative is useful for a medical treatment of cardiac arrhythmias.
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